Mexiletine as an Adjuvant Analgesic for the Management of Neuropathic Cancer Pain

Pharmacological Management of Cancer-Related Pain

“…166 Mexililetine, an oral cogener of lidocaine, has been used after lidocaine infusions. 167 Clinical trial results suggest that mexiletine has a distinct adverse-event profile and may not be tolerated by all patients. 168 …”

Stereospecific Synthesis of m-Hydroxymexiletine Enantiomers

“…This occurs in diseased tissues, rather than under conditions of physiological excitability (tonic block). Its primary use has been the treatment of ventricular arrhythmias, but it can also be used in chronic pain [6][7][8][9] and myotonia [10][11][12]. Mexiletine was clinically used as a racemic mixture; nowadays, the use and commerce of mexiletine hydrochloride (Mexitil, Boehringer Ingelheim) in Italy has been discontinued, because high doses caused drowsiness, confusion, nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, atrioventricular heart block, ventricular arrhythmias, asystole, cardiovascular collapse, and coma [13,14].…”

Mexiletine has a local anesthetic effect on sciatic nerve blockade in rats

“…Mexiletine is an antiarrhythmic drug that has Na 1 channel blocking activity [Kowey et al, 2000] and has been widely used in the treatment of symptomatic and/ or life threatening ventricular arrhythmias, e.g., ventricular tachycardia [Campbell and Williams, 2001;Kowey, 1998;Kowey et al, 2000] and in the treatment of neuropathic pain including diabetic neuropathy, neuropathic cancer pain, among others [Jarvis and Coukell, 1998;Sloan et al, 1999]. Although mexiletine has been used clinically for more than 30 years [Labbé and Turgeon, 1999], its potential clinical use has not been fully explored, e.g., local anesthetic effect.…”

“…Secondly, mexiletine has anticonvulsant activity and is effective in protecting the brain from ischemic insults [Hewitt et al, 2001;Stys and Lesiuk, 1996]. Thirdly, mexiletine potentiates the analgesic effects of opioids and has been used in the treatment of neuropathic pain of multiple origins [Jarvis and Coukell, 1998;Sloan et al, 1999]. The aim of the present study was to evaluate the local anesthetic effects of mexiletine as assessed by sciatic nerve blockade.…”